Parakeratosis inhibitor, pore-shrinking agent and skin preparation for external use

Abstract

It is intended to provide a substance having an effect of shrinking pores by analyzing the mechanism of making pores perceptible and compositions such as a skin preparation for external use which exerts the above effect to thereby make pores imperceptible. As means for solving these problems, there are provided a parakeratosis inhibitor and a pore-shrinking agent comprising an antagonist to an excitatory cell receptor, for example, a glutamate receptor such as N-methyl-D-aspartic acid receptor or an ATP receptor such as P2X receptor, or an agonist to an inhibitory cell receptor such as a γ-aminobutyrate receptor such as bicuculline-sensitive receptor having the Cl— channel therein or glycine receptor, as well as a skin preparation for external use aiming at inhibiting parakeratosis and a skin preparation for external use aiming at shrinking pores each containing such an antagonist to an excitatory cell receptor or an agonist to an inhibitory cell receptor as described above. Owing to the effects of inhibiting parakeratosis and shrinking pores, the skin can be maintained in a healthy state without perceptible pores.

1 . A parakeratosis inhibitor comprising an antagonist to an excitatory cell receptor or an agonist to an inhibitory cell receptor.  
     
     
         2 . The parakeratosis inhibitor according to  claim 1 , wherein the excitatory cell receptor is a glutamic acid receptor or an ATP receptor.  
     
     
         3 . The parakeratosis inhibitor according to  claim 2 , wherein the glutamic acid receptor is an N-methyl-D-aspartic acid receptor.  
     
     
         4 . The parakeratosis inhibitor according to  claim 3 , wherein the antagonist to the N-methyl-D-aspartic acid receptor is dizocylpin or D-glutamic acid.  
     
     
         5 . The parakeratosis inhibitor according to  claim 2 , wherein the ATP receptor is a P2X receptor.  
     
     
         6 . The parakeratosis inhibitor according to  claim 5 , wherein the antagonist to the ATP receptor is suramin, pyridoxal phosphate-6-azophenyl-2′,4′-disulfonic acid or trinitrophenyl-ATP.  
     
     
         7 . The parakeratosis inhibitor according to  claim 1 , wherein the inhibitory cell receptor is a γ-aminobutyric acid receptor or a glycine receptor.  
     
     
         8 . The parakeratosis inhibitor according to  claim 7 , wherein the γ-aminobutyric acid receptor is a Cl— channel-involving bicuculline sensitive receptor.  
     
     
         9 . The parakeratosis inhibitor according to  claim 8 , wherein the agonist to the Cl— channel-involving bicuculline sensitive receptor is γ-aminobutyric acid, muscimol or isogubacin.  
     
     
         10 . The parakeratosis inhibitor according to  claim 7 , wherein the agonist to the glycine receptor is glycine.  
     
     
         11 . A parakeratosis inhibitory skin preparation for external use comprising an antagonist to an excitatory cell receptor or an agonist to an inhibitory cell receptor.  
     
     
         12 - 16 . (canceled)  
     
     
         17 . The parakeratosis inhibitory skin preparation for external use according to  claim 11 , wherein the excitatory cell receptor is a glutamic acid receptor or an ATP receptor.  
     
     
         18 . The parakeratosis inhibitory skin preparation for external use according to  claim 11 , wherein the antagonist to the excitatory cell receptor is dizocylpin, D-glutamic acid, suramin, pyridoxal phosphate-6-azophenyl-2′,4′-disulfonic acid or trinitrophenyl-ATP.  
     
     
         19 . The parakeratosis inhibitory skin preparation for external use according to  claim 11 , wherein the inhibitory cell receptor is a γ-aminobutyric acid receptor or a glycine receptor.  
     
     
         20 . The parakeratosis inhibitory skin preparation for external use according to  claim 11 , wherein the agonist to the inhibitory cell receptor is a γ-aminobutyric acid, muscimol, isogubacin or glycine.  
     
     
         21 . A pore-shrinking preparation comprising an antagonist to an excitatory cell receptor or an agonist to an inhibitory cell receptor.  
     
     
         22 . The pore-shrinking preparation according to  claim 21 , wherein the excitatory cell receptor is a glutamic acid receptor or an ATP receptor.  
     
     
         23 . The pore-shrinking preparation according to  claim 22 , wherein the glutamic acid receptor is an N-methyl-D-aspartic acid receptor.  
     
     
         24 . The pore-shrinking preparation according to  claim 23 , wherein the antagonist to the N-methyl-D-aspartic acid receptor is dizocylpin or D-glutamic acid.  
     
     
         25 . The pore-shrinking preparation according to  claim 22 , wherein the ATP receptor is a P2X receptor.  
     
     
         26 . The pore-shrinking preparation according to  claim 25 , wherein the antagonist to the ATP receptor is suramin, pyridoxal phosphate-6-azophenyl-2′,4′-disulfonic acid or trinitrophenyl-ATP.  
     
     
         27 . The pore-shrinking preparation according to  claim 21 , wherein the inhibitory cell receptor is a γ-aminobutyric acid receptor or a glycine receptor.  
     
     
         28 . The pore-shrinking preparation according to  claim 27 , wherein the γ-aminobutyric acid receptor is a Cl— channel-involving bicuculline sensitive receptor.  
     
     
         29 . The pore-shrinking preparation according to  claim 28 , wherein the agonist to the Cl— channel-involving bicuculline sensitive receptor is γ-aminobutyric acid, muscimol or isogubacin.  
     
     
         30 . The pore-shrinking preparation according to  claim 27 , wherein the agonist to the glycine receptor is glycine.  
     
     
         31 . The pore-shrinking skin preparation for external use comprising an antagonist to an excitatory cell receptor or an agonist to an inhibitory cell receptor.  
     
     
         32 . The pore-shrinking skin preparation for external use according to  claim 31 , wherein the excitatory cell receptor is a glutamic acid receptor or an ATP receptor.  
     
     
         33 . The pore-shrinking skin preparation for external use according to  claim 31 , wherein the antagonist to the excitatory cell receptor is dizocylpin, D-glutamic acid, suramin, pyridoxal phosphate-6-azophenyl-2′,4′-disulfonic acid or trinitrophenyl-ATP.  
     
     
         34 . The pore-shrinking skin preparation for external use according to  claim 31 , wherein the inhibitory cell receptor is a γ-aminobutyric acid receptor or a glycine receptor.  
     
     
         35 . The pore-shrinking skin preparation for external use according to  claim 31 , wherein the agonist to the inhibitory cell receptor is γ-aminobutyric acid, muscimol, isogubacin or glycine.